Yi-Ju Ko, Shing-Ming Cheng, Li-Wen Chang, Hsiang-Fa Liang, Maggie Lu
Drug Delivery Lab, Biomedical Technology and Device Research Laboratories Industrial Technology Research Institute, Hsinchu, TAIWAN MaggieLu@itri.org.tw
The blood-brain barrier (BBB) formed by brain capillary endothelial cells (ECs) highly restricts the applications of many CNS drugs. Most molecules can cross the BBB only via specific endogenous transport systems within the ECs. Here we investigate the capability of BP02 peptide, which was selected from a phage-display peptide library, to facilitate liposome transportation across the BBB and deliver dyes or drugs into the brain. The in vitro performance on cellular binding and BBB permeability demonstrates its potential as a braintargeting ligand. Furthermore, BP02 peptideengrafted liposomes (BP02-Lip) not only could be detected in the brain using an in vivo fluorescence imaging system, but also showed the analgesic efficacy in the hot-plate animal model. Therefore, BP02 peptide has the characteristics essential for BBB-crossing and the potential as a ligand in a brain-specific drug delivery system.